Drugs that I always see and never know... Flashcards
Cyclophosphamide: MOA, use
- alkylating agent that cross-links DNA ==> apoptosis
- uses
- non-Hodgkin’s lymphoma
- breast/ovarian cancer
Naloxone
MOA: mu-opiod receceptor antagonist
use: opiod/heroin overdose
Flumazenil
- MOA:
- use: benzodiazepine antagonist/overdose
Haloperidol
- MOA:
- Use
- anti-psychotic
- delirium
- tranquilization in agitated patient
Lorazepam
- Benzodiazepine
- MOA: allosteric modification of a specific kind of neurotransmitter receptor, the GABAA receptor, which increases the overall conductance of these inhibitory channels
- Use:
- acute anxiety
- status epilepticus
Morphine: MOA
- agonist @ Mu opioid receptors
- Mu opoid receptors = GPCR ==>
- activation of K channels ==> increased K efflux
- ==> hyperpolarization ==> termination of pain signaling from nerves
Isoproteronol MOA
- agonist at B1 and B2 receptors w/no alpha receptor activity ==>
- increase in cardiac contractility (B1)
- vascular smooth muscle relaxation (B2)
Tx of acute mania
- mood stabilizers = lithium, valproate, carbamazepime
- atypical antipsychotic = olanzapine
colchicine: MOA/use/SE
- inhibition of microtubular polymerization ==> prevention of aggregration ==> disrupts chemotaxis and phagocytosis
- also inhibits formation of leukotriene B4
- use = acute gouty arthritis
- SE = nausea, abdominal pain, diarrhea
Enoxaparin: MOA
- low molecular weight heparin
- MOA: binding and activating antithrombin III
- active ATIII prevents factor Xa from: prothrombin ==> thrombin
- ==> anticoagulant effect
Digoxin clearance
via kidneys
Glucorticoids stimulate…?
liver (gluconeogenesis/glycogenolysis)
Valproate during pregnancy ==> ?
- neural tube defects due to inhibition of folic acid absorption @ intestine
- meningocele, spina bifida, etc.
Ebstein’s anomaly association/presentation
- “Ebstein’s anomaly” = “atrialization” of R ventricle due to downward displacement of tricuspid valve
- associated w/mother use of lithium during early pregnancy
Tx/recommendations after total gastrectomy
- parental B12
- to avoid dumping syndrome (colicky ab pain, nausea, diarrhea)
- small meals
- low dietary intake of simple sugars
Isoniazid side effects
- peripheral neuropathy (if given w/pyroxidine)
- hepatotoxicity
- usually mild ==> transient elevated AST, ALT
- elevated bilirubin
- fever, anorexia, nauseau
- severe ==> liver dysfxn, jaundice, bilirubinuria
Hib vaccine + importance
- composed of polyribosyl-ribotol-phosphate (PRP) = component of Hib capsule
- [conjugated w/diptheria or tetanus toxoid]
- ==> lasting immunity against Hib in children
- H. flu ==> epiglottitis
Raloxifene: MOA
- SERM
- estrogen agonist @ bone ==> prevention of osteoporosis
- estrogen antagonist @ breast ==> prevention of breast cancer
Atenolol: MOA + effects
- B1 receptor antagonist
- @ cardiac tissue and JGA, but not @ vascular smooth muscle
- ==> decreased cAMP @ cardiac/renal
Tx of organophosphate poisoning
- Atropine: reversal of muscarinic sx; no effect on nicotinic receptors
- pts still at risk for muscle paralysis
- Pralidoxime: reverses muscarinic and nicotinic effects of organophosphates
- effective only if given early after the exposure
Drug effects:
tachyphylaxis =
additive =
synergistic =
permissive =
- tachy = decreased drug response w/repeated administration
- additive/synergistic = two drugs with similar actions
- additive = admin of both is equal to the sum of the effects
- synergistic = admin of both leads to effects exceeding the sum of the drugs individually
- permissive = admin of a different type of drug (without its own action @ desired site) leads to increased action of an effective drug if given together
AChE in amniotic fluid ==> dx?
- Neural tube defects = failure of fusion of neural tube during 4th week of fetal development
- ==> leakage of fetal CSF ==>
- elevated alpha-fetoprotein
- crosses placenta ==> elevated alpha-fetoprotein @ mother serum
- acetylcholinesterase
- elevated alpha-fetoprotein
Iodine transport @ thyroid
- sodium-iodide symporter brings iodine into thyroid against concentration gradient
- NIS is also responsible for transporting perchlorate and pertechnetate into thyroid
- if potassium perchlorate is present ==> competitive inhibition
Drugs that interfere with iodine uptake
- antithyroid thionamides
- methimazole ==I thyroid peroxidase ==> blocked conversion of iodide to iodine
- propylthiouracil
- usually stopped 7-10 days before tx w/radioactive iodine for hyperthyroidism
Dobutamine impact on pressure-volume loop
- ==> increased contractility
- ==> higher pressures during ventricular ejection phase + greater volume expelled
- ==> widening of P-V loop
Tx for severe asthmatics
- anti-IgE drugs to help reudce allergy triggers of asthma
- e.g. Omalizumab ==> patients w/mod-severe allergic asthma
- IgG1 monoclonal antibody
- binds to IgE to prevent action of IgE w/its receeptor on mast cells ,basophils and other cells
Anti-metabolite drugs
- Folate antagonist
- Methotrexate
- Purine Analogs
- 6-thiopurines
- 6-mercaptopurine
- 6-guanopurine (?)
- Fludarabine ==> CLL tx
- Cladribine ==> HCL tx
- 6-thiopurines
- Pyrimidine Ananologs
- 5-FU
- Capecitabine
- Cytarabine
- Gemcitabine
Vinblastine: MOA, SE
- MOA:
- inhibits MT formation of mitotic spindle
- SE:
- alopecia
- constipation
- myelosuppression
- neurotoxicity (rare)
Cancer drugs that act in the M phase of the cell cycle
- vinca alkaloids=inhibit MT fxn/spindle formation
- vincristine
- vinblastine
- paclitaxel
- binds to tubulin and hyperstabilizes MTs that have already polymerized ==> prevents spindle breakdown
5-fluorouracil: MOA, use
- anti-metabolite
- prevents formation of thymidine vua inhibition of thymidylate synthase
- uses
- slow-growing solid tumors:
- breast
- ovarian
- pancreatic
- colorectal
- gastric carcinomas
6-mercaptopurine: MOA, use
- anti-metabolite
- inhibits formation of purines
- use = cancer drug
Methotrexate: MOA, use
- anti-metabolite
- inhibts dihydrofolate reductase ==> inhibition of DNA synthesis (via same pathway as 5-fluorouracil)
- use = cancer drug
Busulfan: MOA, use
- DNA alkylating agent (cell cyle nonspecific)
- use = CML
Bleomycin: MOA, use, SE
- inhibit replication by inducing DNA strand breaks via free radical formation
- strand breakage interrupts G2 phase of cell cycle (after DNA synthesis)
- uses: testicular tumors, lymphomas, squamous cell carcinoma
- SE
- rales, cough
- infiltration ==> fibrosis
Cyclophosphamide: MOA, uses, SE
- DNA alkylating agent (cell cycle nonspecific)
- activated by CYP450
- ==> apoptosis via DNA crosslinking
- uses
- leukemias, lymphomas
- testicular and gyn cancers
- SE
- hemorrhagic cystitis
How to prevent major side effect of cycloposphamide
- prevent hemorrhagic cystitis via:
- adequate hdration
- IV injection of mesna
Methotrexate rescue
- folinic acid aka n-formyl-xxxx aka leucovorin
- acts synergystically with 5FU
Common method of chemotherapy resistance
- human multi-drug resistance gene (MDR1)
- p-glycoprotein = transmembrane ATP-dependent efflux pump
- broad specificity for hydrophobic compounds
- decreases drug entry and increases efflux
Diuretic overuse impact on blood pH/gases
- diuretic overuse ==> compensatory increase in aldosterone
- aldosterone ==> sodium + H2O retention + K+ and H+ loss @ kidneys ==> metabolic alkalosis
- “contraction alkalosis”
- labs = high pH, high HCO3, high pCO2
Characteristics of drugs w/various volume of distribution
- low Vd = 3-5 L
- highly bound
- charged
- hydrophillic
- high molecular weight
- Vd = 14-16L = plasma + interstitial fluid
- small molecular weight
- hydrophillic
- Vd = 41L = highest distribution
- lipophillic (or hdyro)
- uncharged
Isoniazid: MOA
- antimycobacterial
- inhibits mycolic acid synthesis
Buspirone: MOA/properties, use
- MOA: partial 5HTA1 agonist
- no muscle relaxant
- no anti-seizure
- little hypnosis/hallucinatory
- Use:
- anxiety
- esp. @ previous abusers of anxiolytics
- less addiction potential vs. benzos
a1 receptors location + effect + drugs (agonists)
- pupil sphincter ==> mydriasis (dilation)
- bladder ==> sphincter contraction
- peripheral blood vessels ==> increased SBP
- agonists
- norepi
- epi
- phenylephrine
- methoxamine
beta-1 receptor locations + effects + agonist drugs
- heart ==> increased HR, contractility
- agonsits
- epinephrine
- dobutamine
- dopamine
- isoproteronol
beta-2 receptor locations + effects + agonist drugs
- bronchi ==> bronchodilation
- uterus ==> relaxation
- skeletal muscle bood vessels ==> vasodilation
- agonist drugs
- isproteronal
- terbutaline
- ritodrine
How long till continuous infusion or drug reaches steady state?
- IF: continuous infusion + elimination via first-order kinetics ==>
- steady state plasma concentration @ 4-5 half lives
Presentation of ethylene glycol toxicity
- ethylene glycol metabolized ==> glycolic acid & oxalic acid
- anion-gap metabolic acidosis
- calcium oxalate crystals in urine
- increased osmolar gap
- acute kidney injury/renal failure
- damage to tubular epithelium
- vacuolization
- ballooning
- damage to tubular epithelium
Presentation of theophylline toxicity + tx
- theophylline ==>
- N/V + abdominal pain
- arrhythmias
- seizures **
- Tx
- gastric lavage
- activated charcoal
- cathartics (increase elimination via GI tract)
- beta-blockers ==x arrhythmias
- benzodiazepines & baribituates ==x seizures
Lithium: indications, side effects
- bi-polar; manic and depressive episodes, maintenance
- SE
- DI
- tremor
- hypothyroidism
- Epstein’s anomaly
Valproate: indications, SE
- manic episodes; maintence in bipolar & generalized/absence/myclonic seizures
- SE
- hepatotox
- NTDs
Carbamazepine: indications, SE
- manic episodes, maintence
- partial generalized seizures
- trigeminal neuralgia
- SE
- agranulocytosis
- NTDs
- hyponatremia (SIADH)
Lamotrigine: indications, SE
- depressive episodes, maintenance in bipolar
- focal seizures
- SE
- stevens-johnson
- benign rash
Mood stabilizers in bipolar
- lithium
- valproate
- carbamazepime
- lamotrigine
Use/Effects:
Physostigmine vs. Neostigmin vs. Edrophonium
- all AChE inhibitors
- use = reverse atropine toxicity
- neostigmine/edrophonium = only fxn @ peripherphy; cannot penetrate CNS
- physostigmine = fxns @ periphery & CNS
5HT3-inhibitors
- ondansetron
- granesetron
- dolasetron
Rapid and complete relief in RA [short-term]
glucocorticoids, e.g. prednisone